<sup>99m</sup>Tc-MAG<sub>3</sub>-ASON的制备及其在荷乳腺癌裸鼠中的分布

黄家君; 谢娟; 董孟杰; 李少林

doi:10.13406/j.cnki.cyxb.2005.04.025

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^99mTc-MAG₃-ASON的制备及其在荷乳腺癌裸鼠中的分布

更新时间：2024-01-17

- ^99mTc-MAG₃-ASON的制备及其在荷乳腺癌裸鼠中的分布
- Preparation of ^99m Tc-MAG₃-ASON and distribution in breast carcinoma-bearing nude mouse model
- 重庆医科大学学报 2005年第4期页码：574-577
- 作者机构：
  
  1. 重庆医科大学基础医学院药理学教研室
  2. 重庆医科大学核医学教研室,重庆,400016
- 作者简介：
- 基金信息：
- DOI：10.13406/j.cnki.cyxb.2005.04.025
  中图分类号： R737.9
- 纸质出版日期：2005，
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[1]黄家君,谢娟,董孟杰,李少林.~(99m)Tc-MAG_3-ASON的制备及其在荷乳腺癌裸鼠中的分布[J].重庆医科大学学报,2005(04):574-577+624.

HUANG Jiajun, et al. Preparation of ^99m Tc-MAG₃-ASON and distribution in breast carcinoma-bearing nude mouse model[J]. Journal of Chongqing Medical University, 2005,(4):574-577.
[1]黄家君,谢娟,董孟杰,李少林.~(99m)Tc-MAG_3-ASON的制备及其在荷乳腺癌裸鼠中的分布[J].重庆医科大学学报,2005(04):574-577+624. DOI： 10.13406/j.cnki.cyxb.2005.04.025.

HUANG Jiajun, et al. Preparation of ^99m Tc-MAG₃-ASON and distribution in breast carcinoma-bearing nude mouse model[J]. Journal of Chongqing Medical University, 2005,(4):574-577. DOI： 10.13406/j.cnki.cyxb.2005.04.025.

摘要

目的:探讨99mTc标记的反义寡核苷酸（ASON）的制备及其在荷乳腺癌裸鼠中的分布。方法:一步法合成巯基乙酰三甘氨酰-N-羟基琥珀酰亚胺酯（NHS-MAG3）

并与c-erbB2 mRNA互补的5’末端氨基修饰的15个碱基的ASON偶联;随后进行99mTc的标记

并用Sephadex G25分离纯化99mTc-MAG3-ASON

并评价其稳定性;最后检测其在荷乳腺癌BALB/c裸鼠体内的分布。结果:99mTc-MAG3-ASON平均标记率为70.6%;纯化后

在室温下放置4h

其放化纯度为94.3%;与人血清孵育后

其放化纯度为93.8%;与血浆蛋白结合率为11.8%。乳腺癌组织的摄取率2h达峰值（6.09%ID/g）。结论:以NHS-MAG3为螯合剂制备的99mTc-MAG3-ASON具有良好的稳定性

在乳腺癌部位高浓聚

可望用于肿瘤的显像诊断和治疗。

Abstract

Objective:To discuss the preparation of

99m

Tc-labelled antisense oligonucleotide （ASON） and its distribution in breast carcinoma-bearing nude mouse model.Methods:N-hydroxysuccinimide ester of mercaptoacetylglycylglycylglycine （NHS-MAG

） was synthesized by one step.A 15-mer single-stranded phosphorothioate ASON complementary to c-erbB2 oncogene mRNA was coupled with NHS-MAG

and labelled with

99m

Tc subsequently.

99m

Tc-MAG

-ASON was purified on a gel filtration column of Sephadex G25

then its stability was evaluated

and finally the distribution was detected in breast carcinoma-bearing nude mice model.Results: The average labeling efficiency of 99mTc-MAG

-ASON was 70.6%

and the radiochemical purity was 94.3% after being labelled at room temperature for 4h. When incubated with fresh human serum

the radiochemical purity of

99m

Tc-MAG

-ASON was 93.8%. The serum protein binding of

99m

Tc-MAG

-ASON was 11.8%.The highest uptake of breast carcinoma was 6.09%ID/g at 2hs.Conclusion:

99m

Tc-MAG

-ASON has desirable stability

higher uptake in breast carcinoma and may provide a new sensitive tool for diagnostic imaging and therapy for breast carcinoma in the future.

关键词

乳腺癌反义寡核苷酸（ASON）巯基乙酰三甘氨酸（MAG3）c-erbB299mTc-MAG3-ASON

Keywords

breast carcinomaAntisense oligonucleotide (ASON)Mercaptoacetylglycylglycylglycine （MAG3）c-erbB299m Tc-MAG3-ASON

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99mTc-MAG3-ASON的制备及其在荷乳腺癌裸鼠中的分布

Preparation of 99m Tc-MAG3-ASON and distribution in breast carcinoma-bearing nude mouse model

DOI：10.13406/j.cnki.cyxb.2005.04.025

摘要

Abstract

关键词

Keywords

references

^99mTc-MAG₃-ASON的制备及其在荷乳腺癌裸鼠中的分布

Preparation of ^99m Tc-MAG₃-ASON and distribution in breast carcinoma-bearing nude mouse model